mPEG-icariin nanoparticles for treating myocardial ischaemia

Abstract

Icariin (ICA), a major active ingredient from Chinese medicine, has unique pharmacological effects on ischaemic heart disease. However, its hydrophobic property limits its administration and leads to poor efficacy. This work aimed to change its hydrophobic property and improve the treatment efficacy. We designed a new nano-drug to increase the ICA delivery. ICA was modified with hydrophilic polyethylene glycol monomethyl ether (mPEG) by a succinic anhydride linker to form a polyethylene glycol-icariin (mPEG-ICA) polymer. The structure of this polymer was identified by Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The content of ICA in the polymer was 32% as detected by ultraviolet spectrophotometry. mPEG-ICA nanoparticles, of 143.3 nm, were prepared by the dialysis method, and zeta potential was 0.439 mV by dynamic light scattering. The nanoparticles had a spherical shape on transmission electron microscopy. In media with pH 7.4 and 6.8, ICA release from mPEG-ICA nanoparticles after 72 h was about 0.78% and 64.05%, respectively, so the ICA release depended on the release media pH. On MTT and lactate dehydrogenase activity assay, mPEG-ICA nanoparticles could reduce cell damage induced by oxgen-glucose deprivation. Hoechst 33258 staining and TUNEL and AnnexinV-FITC/PI double staining showed that ICA nanoparticles could increase the activity of H9c2 cardiomyocytes under oxgen-glucose deprivation conditions by decreasing apoptosis. ICA modified by hydrophilic mPEG could improve its efficacy.

RETRACTED: Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells

“…In the dialysis bag method, pre-weighed samples of pure-ICA and ICA-phytosomes (equivalent to 1 mg ICA) were introduced separately into two pre-soaked dialysis bags (molecular weight cut-off (MWCO) of -14 KDa; Sigma-Aldrich, St. Louis, Missouri, USA). The release was performed in 100 mL of phosphate-buffered saline (PBS) buffer pH 7.4 at 37 ± 0.5 • C with continuous stirring at 100 rpm using a magnetic stirrer [35]. Samples were withdrawn at time points of 0.5, 1, 2, 4, 6, 8, and 12 h and immediately replaced with equivalent amount of fresh medium.…”

Icariin Ameliorates Diabetic Cardiomyopathy Through Apelin/Sirt3 Signalling to Improve Mitochondrial Dysfunction

“…Many studies have demonstrated that icariin, a polyphenol flavonoid (Meng et al, 2015), protects cardiomyocytes from injury and, therefore, elicits cardioprotective effects (Ke et al, 2015;Zheng et al, 2019). Interestingly, we found that icariin restored the cardiac function in DCM, as demonstrated by the decrease in LVEF and LVFS ( Figures 1A, B) and the evident increase in LVEDD and LVESD ( Figures 1C, D).…”

Baicalein Ameliorates Myocardial Ischemia Through Reduction of Oxidative Stress, Inflammation and Apoptosis via TLR4/MyD88/MAPKS/NF-κB Pathway and Regulation of Ca2+ Homeostasis by L-type Ca2+ Channels

“…H9c2 cardiomyocytes were digested with 0.25 g/L trypsin (Gibco) at approximately 80% cell confluence to be used for subculturing (Y. Zheng et al, 2019 ). The cells were seeded in 25-cm 2 culture flasks and passaged every 3 days.…”

“…The cells were observed and photographed immediately under fluorescence microscopy (Leica, Germany) (Y. Zheng et al, 2019 ). Nuclei with brightly stained and bright fragments were regarded as apoptotic cells, while cells with blue chromatin and organized structure were considered to be normal.…”